Field of Invention
The present invention provides new hydroxysafflor yellow pharmaceutical salts, in particular new pharmaceutically acceptable salt of hydroxysafflor yellow A, preparation method thereof, lyophilized powder for injection and medical uses thereof. It relates to the field of pharmaceutical chemistry.
Description of Related Arts
Chinese medicine safflower is dried flower of Carthamus tinctouius L., which is a common Chinese medicine for activating blood and dissipating blood stasis, and is applicable for treating blood circulation disorders such as coronary heart disease and angina pectoris. Hydroxysafflor yellow A is a compound with a mono-chalcone glycoside structure, and is a water-soluble portion of the safflower with the most effective pharmacological effect, which can inhibit platelet aggregation and release induced by platelet activating factors, and competitively inhibit combination of the platelet activating factor and the platelet receptor. Therefore, the hydroxysafflor yellow A is an effective ingredient of the safflor yellow for activating blood and dissipating blood stasis. According to research results, the hydroxysafflor yellow A has many pharmacological effects on cardiovascular such as anticoagulant, promoting fibrinolysis, anti-thrombosis, and improving microcirculation.
As the component with the highest content in hydroxysafflor yellow, hydroxysafflor yellow A has been demonstrated pharmaceutically valuable in the treatment of cardiovascular diseases. This mechanism of action is also well known. A number of manufacturing processes of hydroxysafflor yellow A have already been disclosed in present technology, including steps such as using safflower as the raw material, extraction with water, macroporous adsorptive resin separation, dextran gel chromatography, and ultrafiltration, so as to yield hydroxysafflor yellow A for injection. However, hydroxysafflor yellow A prepared by present manufacturing process does not have adequate purity, and generally contains over 10% of impurities. And structure and property of such impurities have not been characterized yet. Therefore, there is certain uncontrollability in terms of quality, and the product may be influenced, in particular stability and safety of medicine for injection. CN102675379A disclosed a method for extracting and refining hydroxysafflor yellow A from safflower, in particular five steps including extraction from traditional Chinese medicine safflower, purifying through weak-base ion exchange resin, purifying through neutral polarity macroporous adsorptive resin, purifying through non-polar macroporous adsorptive resin, and lyophilization, which only yields over 80% of hydroxysafflor yellow A.